Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/323)
-
Publication number: 20150057248Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.Type: ApplicationFiled: September 1, 2014Publication date: February 26, 2015Applicant: The Board of Regents of The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
-
Publication number: 20150056213Abstract: Disclosed are selective histone deactylase inhibitors (HDACi) that having Formula (I). Methods of making and using these inhibitors for the treatment of cancer, in particular melanoma are also disclosed.Type: ApplicationFiled: March 7, 2013Publication date: February 26, 2015Inventors: Eduardo M. Sotomayor, Joel Bergman, Alan Kozikowski, Karrune Veeraprasert Woan, Alejandro V. Villagra
-
Publication number: 20150045391Abstract: A combination of filanesib and pomalidomide for treating patients is provided.Type: ApplicationFiled: August 7, 2014Publication date: February 12, 2015Inventors: Deborah A. Anderson, Michael J. Humphries, Robert A. Rieger, Lance M. Williams
-
Publication number: 20150038484Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Applicant: PFIZER INC.Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
-
Patent number: 8946265Abstract: The present invention relates to improved processes for preparing 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.Type: GrantFiled: March 1, 2010Date of Patent: February 3, 2015Assignee: Generics [UK] LimitedInventors: Vinayak Govind Gore, Vinay Kumar Shukla, Shreyas Shrikant Bhandari, Suresh Hasbe
-
Patent number: 8940784Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: GrantFiled: February 2, 2007Date of Patent: January 27, 2015Assignee: Syntarga B.V.Inventors: Patrick Henry Beusker, Franciscus Marinus Hendrikus de Groot, Lutz F. Tietze, Felix Major, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker
-
Publication number: 20150025089Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
-
Publication number: 20150018389Abstract: A method for treating a central nervous system or peripheral nervous system dopaminergic deficit state in a mammalian organism in need of such treatment, said method comprising administering to said mammal an amount of thalidomide effective in the treatment of a dopaminergic deficit state and for a time sufficient to achieve a suitable blood level to treat said dopaminergic deficit state.Type: ApplicationFiled: July 12, 2013Publication date: January 15, 2015Inventor: Marilyn Andrulis
-
Publication number: 20150018310Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: September 29, 2014Publication date: January 15, 2015Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
-
Publication number: 20150011557Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.Type: ApplicationFiled: September 7, 2012Publication date: January 8, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
-
Publication number: 20150010619Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: September 26, 2014Publication date: January 8, 2015Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
-
Patent number: 8927725Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein A, B and D are each oxygen or sulfur, provided that least one of A, B and D is sulfur; and R1-R8 are each independently hydrogen, hydroxyl, acyl, substituted acyl, acyloxy, substituted acyloxy, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, amino, substituted amino, halogen, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, or a thio-containing group.Type: GrantFiled: December 2, 2011Date of Patent: January 6, 2015Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Nigel H. Greig, Weiming Luo, David Tweedie, Harold W. Holloway, Qian-Sheng Yu, Edward J. Goetzl
-
Publication number: 20150005279Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 26, 2014Publication date: January 1, 2015Applicant: ABBVIE INC.Inventors: Dominique Bonafoux, Heather M. Davis, Kristine E. Frank, Michael M. Friedman, J. Martin Herold, Michael Z. Hoemann, Raymond Huntley, Augustine Osuma, George Sheppard, Gagandeep K. Somal, Jennifer Van Camp, Stacy A. Van Epps, Anil Vasudevan, Grier A. Wallace, Lu Wang, Lu Wang, Zhi Wang, Noel S. Wilson, Xiangdong Xu
-
Publication number: 20150005303Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Inventors: George W. MULLER, Roger Shen-Chu CHEN, Alexander L. RUCHELMAN
-
Publication number: 20150005346Abstract: The present invention relates to novel heterocyclic derivatives which are allosteric modulators of cannabinoid receptor 1 (CB1) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with endocannabinoid dysfunction and diseases in which the CB1 subtype of cannabinoid receptor is involved; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.Type: ApplicationFiled: July 3, 2014Publication date: January 1, 2015Inventors: Ganeshsingh A. THAKUR, Pushkar M. KULKARNI
-
Patent number: 8921559Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: November 30, 2011Date of Patent: December 30, 2014Assignee: Janssen Pharmaceutica NVInventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
-
Patent number: 8912199Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: October 21, 2013Date of Patent: December 16, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
-
Publication number: 20140364393Abstract: The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.Type: ApplicationFiled: December 5, 2012Publication date: December 11, 2014Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
-
Patent number: 8907097Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: GrantFiled: October 30, 2009Date of Patent: December 9, 2014Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
-
Publication number: 20140349965Abstract: Disclosed herein are compositions and methods for treating neoplastic diseases. Included are compositions and methods that are effective against multiple myeloma cells resistant to conventional and bortezomib treatment. Furthermore, combination treatment with two different proteosome inhibitors is shown to be synergistic for treating multiple myeloma.Type: ApplicationFiled: March 25, 2014Publication date: November 27, 2014Applicants: Dana-Farber Cancer Institute, Inc., Triphase Research and Development I Corp.Inventors: Kenneth C. Anderson, Dharminder Chauhan, Michael A. Palladino
-
Publication number: 20140343001Abstract: The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy.Type: ApplicationFiled: December 19, 2012Publication date: November 20, 2014Applicant: Universita di PisaInventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Valeria Di Bussolo, Gino Giannaccini, Antonio Lucacchini, Paul J. Hergenrother, Emilia C. Calvaresi
-
Publication number: 20140343037Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
-
Patent number: 8889674Abstract: The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted monocyclic aryl or monocyclic heterocyclyl; X is a single bond or C(?O); Y is a single bond, CR5R6NR7 or C(?O)NR7; R1 and R2 are independently hydrogen or substituted or unsubstituted alkyl; R3 is substituted or unsubstituted aryl or heterocyclyl; R4 is halogen, substituted or unsubstituted alkyl, alkoxy, aryloxy or heterocyclyloxy, etc.; p is an integer of 0 to 2; q is 0 or 1; m is 0 or 1; n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or bicyclic fused hetero ring.Type: GrantFiled: March 5, 2010Date of Patent: November 18, 2014Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Sakagami, Hitomi Araki, Hiroshi Hashizume, Hiroshi Yari, Kenji Takaya
-
Patent number: 8889716Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: GrantFiled: May 7, 2012Date of Patent: November 18, 2014Assignee: CHDI Foundation, Inc.Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
-
Publication number: 20140336223Abstract: Pharmaceutical compositions and single unit dosage forms of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer or an inflammatory disease.Type: ApplicationFiled: July 30, 2014Publication date: November 13, 2014Inventors: Anthony J. TUTINO, Michael T. KELLY
-
Publication number: 20140328913Abstract: The present invention relates to an improved gelatinous coated dosage form having two end regions coated with gelatinous materials and an exposed circumferential band. Openings are provided in at least the exposed band to reveal the core material. The invention also relates to methods for manufacturing such gelatinous coated dosage forms.Type: ApplicationFiled: July 18, 2014Publication date: November 6, 2014Inventors: Roger A. Rinker, Nicholas J. Casale, James H. Comly, Brenda Pollack, Johan Geerke, Martin Costello, Dennis Wieand, Kishor Parekh
-
Patent number: 8877932Abstract: Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1, 3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed.Type: GrantFiled: March 8, 2010Date of Patent: November 4, 2014Assignee: Natco Pharma LimitedInventors: Durga Prasad Konakanchi, Buchappa Gongalla, Kotayya Babu Sikha, Chandrasekar Kandaswamy, Kali Satya Bhujanga Rao Adibhatla, Venkaiah Chowdary Nannapaneni
-
Patent number: 8877780Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: May 30, 2008Date of Patent: November 4, 2014Assignee: Celgene CorporationInventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman, Hon-Wah Man, Weihong Zhang, Ehab M. Khalil
-
Publication number: 20140315889Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.Type: ApplicationFiled: October 26, 2012Publication date: October 23, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
-
Publication number: 20140315953Abstract: A method for treating migraines is disclosed. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent, including small molecules and peptides being administered to a patient in need of treatment. In particular, the drug delivery system is designed for inhalation for delivery of drugs to the pulmonary circulation in a rapid and therapeutically effective manner.Type: ApplicationFiled: June 16, 2014Publication date: October 23, 2014Inventors: Andrea Leone-Bay, Grayson W. Stowell, Joseph J. Guarneri, Dawn M. Carlson, Marshall Grant, Chad C. Smutney
-
Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
-
Publication number: 20140309195Abstract: Provided herein are small molecules for the induction of fibroblast proliferation and increased secretion or production of proteins. The small molecules described herein can be used for the promotion of skin regeneration. Also provided herein are methods for promoting skin regeneration and wound healing.Type: ApplicationFiled: January 8, 2014Publication date: October 16, 2014Applicant: INTERNATIONAL STEM CELL CORPORATIONInventors: Rodolfo Gonzalez, Maxim Poustovoitov, Ruslan Semechkin
-
DERIVATIVES OF 1-(SUBSTITUTED SULFONYL)-2-AMINOIMIDAZOLINE AS ANTITUMOR AND ANTIPROLIFERATIVE AGENTS
Publication number: 20140309259Abstract: The invention provides novel, water-soluble 2-aminoimidazoline derivatives having general Formula (I) as well as some precursors of Formula (I), which are very potent inducers of G2/M cell cycle arrest. In treated tumor cells, compounds of Formula (I) give gene expression profile distinct from known antimitotic agents. The invention also provides methods for preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.Type: ApplicationFiled: June 17, 2014Publication date: October 16, 2014Inventors: Stanislaw Wieslaw Pikul, Wieslaw Marek Cholody -
DERIVATIVES OF 1-(SUBSTITUTED SULFONYL)-2-AMINOIMIDAZOLINE AS ANTITUMOR AND ANTIPROLIFERATIVE AGENTS
Publication number: 20140309240Abstract: The invention provides novel, water-soluble 2-aminoimidazoline derivatives having general Formula (I) as well as some precursors of Formula (I), which are very potent inducers of G2/M cell cycle arrest. In treated tumor cells, compounds of Formula (I) give gene expression profile distinct from known antimitotic agents. The invention also provides methods for preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.Type: ApplicationFiled: April 9, 2014Publication date: October 16, 2014Inventors: Stanislaw Wieslaw Pikul, Wieslaw Marek Cholody -
Publication number: 20140294767Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Inventors: David Waugh, Christopher Self, Guangtao Zhang, Yves Pommier, Robert H. Shoemaker, Michael Currens, John Cardellina, Andrew Jobson, George Lountos, Dominic Scudiero
-
Publication number: 20140296229Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: March 26, 2014Publication date: October 2, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Harald ENGELHARDT, Davide GIANNI, Andreas MANTOULIDIS, Christian SMETHURST
-
Publication number: 20140294979Abstract: Methods and pharmaceutical compositions for regulations of Guanosine- (G-) and/or Guanosine-cytosine-rich (GC-rich) nucleic acid expressions are provided. The methods include a step of interacting the G- and/or GC-rich region of the nucleic acid with thalidomide, and the pharmaceutical compositions include the thalidomide and a pharmaceutical carrier.Type: ApplicationFiled: May 7, 2014Publication date: October 2, 2014Applicant: National Yang-Ming UniversityInventor: Rong-Tsun Wu
-
Publication number: 20140296212Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: February 10, 2014Publication date: October 2, 2014Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Allison L. Zulli, Brigitte Lesur, Babu G. Sundar, Christophe Yue
-
Publication number: 20140296292Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.Type: ApplicationFiled: November 12, 2012Publication date: October 2, 2014Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
-
Publication number: 20140296327Abstract: This disclosure provides methods for surveillance, early detection and diagnosis, subtype classification, prediction of recurrence, prognosis and therapy of malignant mesothelioma based on profiles of indicator mutations in disclosed genes.Type: ApplicationFiled: October 24, 2012Publication date: October 2, 2014Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Raphael Bueno, David Sugarbaker
-
Publication number: 20140296202Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: October 18, 2012Publication date: October 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
-
Publication number: 20140296291Abstract: The invention relates to novel crystalline forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.Type: ApplicationFiled: June 7, 2012Publication date: October 2, 2014Inventors: Scott L. Childs, Shreenivas R. Lingireddy, Nathan Barishansky
-
Publication number: 20140296217Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.Type: ApplicationFiled: February 20, 2014Publication date: October 2, 2014Applicant: Boehringer Ingelheim International GmbHInventors: John Edward PARK, Gerald Juergen ROTH, Armin HECKEL, Nveed CHAUDHARY, Trixi BRANDL, Georg DAHMANN, Matthias GRAUERT
-
Patent number: 8846930Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.Type: GrantFiled: November 23, 2011Date of Patent: September 30, 2014Assignee: Pierre Fabre MedicamentInventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
-
Patent number: 8846684Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.Type: GrantFiled: March 19, 2012Date of Patent: September 30, 2014Assignee: The Regents of The University of MichiganInventors: Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
-
Patent number: 8841295Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: November 3, 2006Date of Patent: September 23, 2014Assignee: Panmira Pharmaceuticals, LLCInventors: John H. Hutchinson, Yiwei Li, Mustapha Haddach, Nicholas Simon Stock
-
Patent number: 8841325Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.Type: GrantFiled: November 24, 2010Date of Patent: September 23, 2014Assignee: Celgene CorporationInventors: Carole Brosseau, Justin Blake Bartlett, Angus George Dalgleish, Kay Winifred Colston, Christine Galustian
-
Publication number: 20140274953Abstract: The described invention provides an ex vivo dynamic multiple myeloma (MM) cancer niche contained in a microfluidic device. The dynamic MM cancer niche includes (a) a three-dimensional tissue construct containing a dynamic ex vivo bone marrow (BM) niche, which contains a mineralized bone-like tissue containing viable osteoblasts self-organized into cohesive multiple cell layers and an extracellular matrix secreted by the viable adherent osteoblasts; and a microenvironment dynamically perfused by nutrients and dissolved gas molecules; and (b) human myeloma cells seeded from a biospecimen composition comprising mononuclear cells and the multiple myeloma cells. The human myeloma cells are in contact with osteoblasts of the BM niche, and the viability of the human myeloma cells is maintained by the MM cancer niche.Type: ApplicationFiled: March 14, 2013Publication date: September 18, 2014Inventors: Woo Lee, Jenny Zilberberg, David Samuel Siegel, Peter Tolias, Hongjun Wang, Wenting Zhang
-
Publication number: 20140271638Abstract: Methods of treating, preventing or managing mantle cell lymphomas are disclosed. The methods encompass the administration of an immunomodulatory compound of the invention known as Revlimid® or lenalidomide. The invention further relates to methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods of the invention are also disclosed.Type: ApplicationFiled: May 30, 2014Publication date: September 18, 2014Applicant: Celgene CorporationInventor: Jerome B. Zeldis
-
Publication number: 20140275114Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf ANDERSKEWITZ, Marc GRUNDL, Gerd MORSCHHAEUSER, Thorsten OOST, Alexander PAUTSCH